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Status:
Possibly Marketed Outside US
Source:
Alexidine by Chemos GmbH
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Alexidine dihydrochloride, an antibacterial compound, which is used during endodontic procedures. It is a dibiguanide ahent and is effective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1). It was noted that PTPMT1 could serve as a pharmacological target in the treatment of type II diabetes. Alexidine dihydrochloride is also an apoptosis-promoting agent possessing the anticancer properties.
Status:
Possibly Marketed Outside US
Source:
Unknown by Nippon Organon|Pfizer
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Lomerizine (INN) (also known as KB-2796) is a diphenylpiperazine class L-type and T-type calcium channel blocker with relatively selective CNS effects. Voltage dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting. The common pharmacological profile of L-type channels is determined by the α1 subunit, which forms the Ca2+ selective. Lomerizine was developed as a potential agent for the selective improvement of the ocular or cerebrovascular circulation with minimal adverse cardiovascular effects, and it is used as an anti- migraine drug. Lomerizine selectively relaxes smooth muscle cells by inhibiting L-type Ca2+ influx, thereby reducing tone and increasing blood flow in cerebral vessels. Lomerizine also shows neuroprotective effects against secondary degeneration resulting from injury in retinal ganglion cells. While some calcium-channel blockers, such as flunarizine, act on the dopaminergic system, lomerizine is ineffective in vivo at inhibiting the release of dopamine. However, it has been observed to weakly inhibit the binding of [3H]spiperone to D2 dopamine receptors in vitro. While researchers are unsure of the reason for this difference, one hypothesis is that the doses administered cannot reach a high enough concentration in the brain to affect D2 receptors.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Vaniprevir (MK-7009) is an non-covalent competitive macrocyclic inhibitor of Hepatitis C virus NS3/4A protease genotype 1a and 1b proteases at subnanomolar concentrations with
modestly shifted potency against genotype 2a and 2b proteases at low nanomolar concentrations. Merck & Co. developed vaniprevir in combination with standard therapy for the twice-daily treatment of hepatitis C virus infections. The product has been launched in Japan under name VANIHEP, and Merck reported in its 2014 annual report that the product will only be available in this region.
Status:
Possibly Marketed Outside US
Source:
Unknown by Fourneau, E.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.
Status:
Possibly Marketed Outside US
Source:
Eumotol by Byk Gulden [W. Germany]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Bumadizone is a non-steroidal anti-inflammatory drug exerting analgesic, antipyretic and anti-inflammatory properties. It has been studied in the treatment of rheumatoid diseases.
Status:
Possibly Marketed Outside US
Source:
NCT00558155: Phase 4 Interventional Completed Gastric Cancer
(2001)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Bunitrolol is a beta-adrenergic antagonist that can be used for treatment of coronary heart disease. It improves cardiac performance after beta-blockade in patients with coronary artery disease. Bunitrolol was found to have a greater beta 1 than beta 2 adrenergic activity and a weak alpha 1 blocking action.
Status:
Possibly Marketed Outside US
Source:
DIBEKACIN MEIJI by Umezawa, H. et al.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dibekacin is a semisynthetic aminoglycoside antibiotic useful in the treatment of severe gram-negative bacterial infections. The drug is marketed in Japan.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Mitoguazone is a guanylhydrazone derivative with potential antineoplastic activity. Mitoguazone inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in a decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. In the 1960s the drug was investigated in clinical trials. Despite the responses in acute leukemia, chronic myelogenous leukemia, lymphoma, multiple myeloma, head and neck cancer, esophageal cancer and other types of cancer, the development of the drug was discontinued because of marked myelosuppression and mucositis. Using a weekly schedule of administration, mitoguazone had minimal toxicity and showed limited activity in patients with lymphoma, esophageal cancer, prostate cancer, and other types of tumors.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zinc picrate is an industrially important material. Metal, including zinc, complexes of picric acid are used in the field of homeopathy.
Status:
Possibly Marketed Outside US
Source:
NCT01998620: Phase 4 Interventional Unknown status Hepatitis B
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
S-Adenosylmethionine (often referred to as SAMe) is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. SAM is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma (HCC), HepG2 cells and colon cancer cells. Because of structural instability, stable salt forms of SAM are required for its use as an oral drug. The commonly used salts: tosylate, butanedisulfonate, disulfate tosylate, disulfate ditosylate, and disulfate monotosylate. SAMe has been marketed in some European countries since the mid-1980s for the treatment of depression and for other medical conditions such as osteoarthritis (joint disease that causes joint pain and stiffness), fibromyalgia (widespread pain and stiffness). In addition, it is used to treat liver disease and migraine headaches. However, it is not formally approved in the UK for the treatment of depression, and in the USA, it is classified only as a dietary supplement. Some research suggests that it is more effective than placebo in treating mild-to-moderate depression and is just as effective as antidepressant medications without the side effects (headaches, sleeplessness, and sexual dysfunction). In addition, antidepressants tend to take 6 to 8 weeks to begin working, while It seems to begin more quickly. Researchers are not sure how SAMe works to relieve depression. But they speculate it might increase the amount of serotonin in the brain just as some antidepressants do. Many studies have examined injectable forms of SAMe, not oral supplements.